IL196601A - 2-morpholine-4-yl (pyrolidino / piperidino) pyrimidine, pharmaceuticals containing them and intermediates in the process of preparation - Google Patents
2-morpholine-4-yl (pyrolidino / piperidino) pyrimidine, pharmaceuticals containing them and intermediates in the process of preparationInfo
- Publication number
- IL196601A IL196601A IL196601A IL19660109A IL196601A IL 196601 A IL196601 A IL 196601A IL 196601 A IL196601 A IL 196601A IL 19660109 A IL19660109 A IL 19660109A IL 196601 A IL196601 A IL 196601A
- Authority
- IL
- Israel
- Prior art keywords
- pyrrolidino
- piperidino
- morpholin
- intermediates
- preparation
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2006216108 | 2006-08-08 | ||
JP2007118631 | 2007-04-27 | ||
PCT/JP2007/065396 WO2008018426A1 (fr) | 2006-08-08 | 2007-08-07 | Dérivé de pyrimidine comme inhibiteur de la PI3K et son utilisation |
Publications (2)
Publication Number | Publication Date |
---|---|
IL196601A0 IL196601A0 (en) | 2009-11-18 |
IL196601A true IL196601A (en) | 2015-03-31 |
Family
ID=39032956
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IL196601A IL196601A (en) | 2006-08-08 | 2009-01-20 | 2-morpholine-4-yl (pyrolidino / piperidino) pyrimidine, pharmaceuticals containing them and intermediates in the process of preparation |
Country Status (26)
Country | Link |
---|---|
US (1) | US8022205B2 (fr) |
EP (1) | EP2050749B1 (fr) |
JP (1) | JP4450857B2 (fr) |
KR (1) | KR101435692B1 (fr) |
AR (1) | AR062292A1 (fr) |
AU (1) | AU2007282535B9 (fr) |
BR (1) | BRPI0714908B8 (fr) |
CA (1) | CA2659604C (fr) |
CL (1) | CL2007002316A1 (fr) |
CY (1) | CY1119882T1 (fr) |
DK (1) | DK2050749T3 (fr) |
ES (1) | ES2657635T3 (fr) |
HU (1) | HUE035116T2 (fr) |
IL (1) | IL196601A (fr) |
LT (1) | LT2050749T (fr) |
MX (1) | MX2009001451A (fr) |
MY (1) | MY145385A (fr) |
NO (1) | NO342978B1 (fr) |
NZ (1) | NZ575274A (fr) |
PE (1) | PE20080527A1 (fr) |
PL (1) | PL2050749T3 (fr) |
PT (1) | PT2050749T (fr) |
RU (1) | RU2448109C2 (fr) |
SI (1) | SI2050749T1 (fr) |
TW (1) | TWI394758B (fr) |
WO (1) | WO2008018426A1 (fr) |
Families Citing this family (67)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2527696T3 (es) * | 2006-12-21 | 2015-01-28 | Nerviano Medical Sciences S.R.L. | Derivados de pirazoloquinazolina sustituidos, procedimientos para su preparación y su uso como inhibidores de la quinasa |
TW200938201A (en) * | 2008-02-07 | 2009-09-16 | Chugai Pharmaceutical Co Ltd | Pyrrolopyrimidine derivative as PI3K inhibitor and use thereof |
CN102137592B (zh) | 2008-06-16 | 2015-01-28 | 田纳西大学研究基金会 | 用于治疗癌症的化合物 |
US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
EP2307414A4 (fr) * | 2008-07-07 | 2011-10-26 | Xcovery Holding Co Llc | Inhibiteurs sélectifs des isoformes de la pi3 kinase |
TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
GB2465405A (en) * | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
CN102264732A (zh) * | 2008-11-11 | 2011-11-30 | 艾科睿控股公司 | PI3K/mTOR激酶抑制剂 |
ES2462715T3 (es) * | 2008-12-19 | 2014-05-26 | Genentech, Inc. | Compuestos y métodos de uso |
MX2011010105A (es) | 2009-03-27 | 2012-01-12 | Pathway Therapeutics Inc | Sulfonamidas de pirimidinilo y 1,3,5-triazinilo benzimidazol y su uso en terapia de cancer. |
WO2010114494A1 (fr) * | 2009-04-03 | 2010-10-07 | S*Bio Pte Ltd | Purines 2-morpholino 8-substituées pour une utilisation en tant qu'inhibiteurs de pi3k et/ou mtor dans le traitement de troubles prolifératifs |
SG10201405826RA (en) | 2009-06-17 | 2014-12-30 | Vertex Pharma | Inhibitors of influenza viruses replication |
CN102482278B (zh) | 2009-06-29 | 2015-04-22 | 因塞特公司 | 作为pi3k抑制剂的嘧啶酮类 |
EP3072890B1 (fr) | 2009-07-07 | 2018-10-17 | MEI Pharma, Inc. | Pyrimidinyl et 1,3,5-triazinyl benzimidazoles et leur utilisation dans la thérapie du cancer |
RU2595718C2 (ru) * | 2009-09-09 | 2016-08-27 | Селджен Авиломикс Рисерч,Инк. | Ингибиторы pi3-киназы и их применение |
US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
CN102883607B (zh) | 2010-03-01 | 2015-07-22 | Gtx公司 | 用于治疗癌的化合物 |
EP2571884A4 (fr) * | 2010-05-19 | 2014-03-19 | Xcovery Holding Co Llc | Inhibiteurs sélectifs de la mtor kinase |
US9096600B2 (en) | 2010-12-20 | 2015-08-04 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
RU2013138835A (ru) * | 2011-02-09 | 2015-03-20 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения в качестве ингибиторов pi3 киназы |
KR101940831B1 (ko) | 2011-03-28 | 2019-01-21 | 메이 파마, 아이엔씨. | (알파-치환된 아르알킬아미노 및 헤테로아릴알킬아미노)피리미딘일 및 1,3,5-트라이아진일 벤즈이미다졸, 이들을 함유하는 약학 조성물, 및 증식성 질병의 치료에 사용하기 위한 이들 화합물 |
WO2013006634A2 (fr) * | 2011-07-05 | 2013-01-10 | Vertex Pharmaceuticals Incorporated | Procédés et intermédiaires pour produire des azaindoles |
UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
HUE053953T2 (hu) | 2011-09-02 | 2021-08-30 | Incyte Holdings Corp | Heterociklusos aminok mint PI3K-gátlók |
US20130123255A1 (en) * | 2011-11-10 | 2013-05-16 | Chugai Seiyaku Kabushiki Kaisha | Combination of a pi3k inhibitor and a mek inhibitor |
EP2788500A1 (fr) | 2011-12-09 | 2014-10-15 | F.Hoffmann-La Roche Ag | Identification de non-répondeurs aux inhibiteurs de her2 |
AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
US10213432B2 (en) | 2012-05-16 | 2019-02-26 | Novartis Ag | Dosage regimen for a PI-3 kinase inhibitor |
CN103450204B (zh) * | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途 |
JP5855250B2 (ja) | 2012-07-02 | 2016-02-09 | 大鵬薬品工業株式会社 | イミダゾオキサジン化合物による抗腫瘍効果増強剤 |
US9145411B2 (en) | 2012-08-02 | 2015-09-29 | Asana Biosciences, Llc | Substituted amino-pyrimidine derivatives |
WO2014068070A1 (fr) | 2012-10-31 | 2014-05-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Procédés pour prévenir le syndrome des antiphospholipides (sapl) |
TR201812261T4 (tr) * | 2012-11-01 | 2018-11-21 | Infinity Pharmaceuticals Inc | Pi3 ki̇naz i̇zoform modülatörleri̇ i̇le kanser tedavi̇si̇ |
CN103588792B (zh) * | 2013-03-04 | 2016-03-23 | 中国科学院上海药物研究所 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
US9242969B2 (en) * | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
US9296727B2 (en) | 2013-10-07 | 2016-03-29 | Vertex Pharmaceuticals Incorporated | Methods of regioselective synthesis of 2,4-disubstituted pyrimidines |
US9656996B2 (en) * | 2013-10-16 | 2017-05-23 | Shanghai Yingli Pharmaceutical Co., Ltd. | Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof |
LT3068782T (lt) | 2013-11-13 | 2018-09-10 | Vertex Pharmaceuticals Incorporated | Gripo virusų replikacijos inhibitorių paruošimo būdai |
WO2015149721A1 (fr) | 2014-04-04 | 2015-10-08 | Crown Bioscience, Inc.(Taicang) | Méthodes permettant de déterminer la sensibilité à des inhibiteurs de mek/erk |
WO2015155624A1 (fr) | 2014-04-10 | 2015-10-15 | Pfizer Inc. | Dérivés de dihydropyrrolopyrimidine |
US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
MD3262046T2 (ro) | 2015-02-27 | 2021-03-31 | Incyte Corp | Săruri de inhibitori ai PI3K și procedee pentru prepararea lor |
JPWO2016136928A1 (ja) | 2015-02-27 | 2017-08-31 | 大鵬薬品工業株式会社 | イミダゾオキサジンの結晶、当該結晶を含む医薬組成物、及び当該結晶の製造方法 |
US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
WO2016183060A1 (fr) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Procédé de synthèse d'un inhibiteur de phospho-inositide 3-kinases |
JP6704416B2 (ja) | 2015-05-13 | 2020-06-03 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | インフルエンザウイルスの複製の阻害剤を調製する方法 |
MA42422A (fr) | 2015-05-13 | 2018-05-23 | Vertex Pharma | Inhibiteurs de la réplication des virus de la grippe |
JP6616244B2 (ja) * | 2015-05-29 | 2019-12-04 | 北興化学工業株式会社 | 新規なヒドロキシフェニルボロン酸エステルとその製造方法、およびヒドロキシビフェニル化合物の製造法 |
US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
DK3458067T3 (da) * | 2016-05-18 | 2021-04-06 | Univ Basel | Behandling af neurologiske lidelser |
EP3481829B1 (fr) | 2016-07-08 | 2021-04-07 | H. Hoffnabb-La Roche Ag | Dérivés fusionnés de pyrimidine |
EP3484884B1 (fr) | 2016-07-14 | 2021-01-27 | Hoffmann-La Roche AG | Dérivés de pyrimidine fusionnés |
IT201600092469A1 (it) * | 2016-09-14 | 2018-03-14 | Lundbeck Pharmaceuticals Italy S P A | Processo per la produzione di Blonanserina |
CN109715163B (zh) | 2016-09-19 | 2022-11-22 | 诺华股份有限公司 | 包含raf抑制剂和erk抑制剂的治疗组合 |
EP3523304B1 (fr) | 2016-10-04 | 2021-01-27 | H. Hoffnabb-La Roche Ag | Dérivés hétéroaryles bicycliques |
IL270224B1 (en) | 2017-05-02 | 2024-04-01 | Novartis Ag | Combination therapy using trametinib and a defined RAF inhibitor |
WO2018217787A1 (fr) | 2017-05-23 | 2018-11-29 | Mei Pharma, Inc. | Polythérapie |
CN111212643A (zh) | 2017-08-14 | 2020-05-29 | 梅制药公司 | 联合疗法 |
WO2019101984A1 (fr) | 2017-11-27 | 2019-05-31 | F. Hoffmann-La Roche Ag | Dérivés de pyrimidine |
WO2021247862A1 (fr) * | 2020-06-03 | 2021-12-09 | Yumanity Therapeutics, Inc. | Hétéroarènes bicycliques et leurs procédés d'utilisation |
TW202220661A (zh) | 2020-08-07 | 2022-06-01 | 德商柏林化學股份公司 | 包含pi3k抑制劑之經改良醫藥調配物 |
CA3215002A1 (fr) | 2021-04-09 | 2022-10-13 | Christian Gege | Inhibiteurs deuteres de dhodh |
KR20240133710A (ko) * | 2021-12-08 | 2024-09-04 | 키네타, 인크. | 피리미딘 및 그의 사용 방법 |
AU2022407047A1 (en) * | 2021-12-08 | 2024-07-25 | Kineta, Inc. | Bicyclic heteroarenes and methods of their use |
WO2024023766A1 (fr) | 2022-07-28 | 2024-02-01 | Berlin-Chemie Ag | Polythérapie à base d'inhibiteur de p13k |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0799617A3 (fr) | 1986-02-24 | 1997-11-12 | Mitsui Petrochemical Industries, Ltd. | Agent thérapeutique pour le traitement des maladies neurologiques |
JPH08325268A (ja) | 1986-02-24 | 1996-12-10 | Mitsui Petrochem Ind Ltd | ピロロ〔3,4−d〕ピリミジン誘導体 |
AU645504B2 (en) * | 1989-10-11 | 1994-01-20 | Teijin Limited | Bicyclic pyrimidine derivative, method of producing the same, and pharmaceutical preparation containing the same as active ingredient |
TW530047B (en) * | 1994-06-08 | 2003-05-01 | Pfizer | Corticotropin releasing factor antagonists |
CA2426654C (fr) * | 2000-10-23 | 2010-12-21 | Smithkline Beecham Corporation | Nouveaux composes |
US7384937B2 (en) * | 2002-11-06 | 2008-06-10 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
ES2375111T3 (es) * | 2002-11-21 | 2012-02-24 | Novartis Ag | Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-quinasa y su uso en el tratamiento de c�?ncer. |
RU2328497C2 (ru) * | 2003-05-05 | 2008-07-10 | Ф.Хоффманн-Ля Рош Аг | Конденсированные производные пиримидина и лекарственное средство, обладающее активностью в отношении crf |
-
2007
- 2007-08-07 RU RU2009108328/04A patent/RU2448109C2/ru active
- 2007-08-07 NZ NZ575274A patent/NZ575274A/en unknown
- 2007-08-07 LT LTEP07792065.0T patent/LT2050749T/lt unknown
- 2007-08-07 EP EP07792065.0A patent/EP2050749B1/fr active Active
- 2007-08-07 BR BRPI0714908A patent/BRPI0714908B8/pt active IP Right Grant
- 2007-08-07 KR KR1020097002650A patent/KR101435692B1/ko active IP Right Grant
- 2007-08-07 SI SI200731994T patent/SI2050749T1/en unknown
- 2007-08-07 DK DK07792065.0T patent/DK2050749T3/en active
- 2007-08-07 PT PT77920650T patent/PT2050749T/pt unknown
- 2007-08-07 MX MX2009001451A patent/MX2009001451A/es active IP Right Grant
- 2007-08-07 US US12/376,039 patent/US8022205B2/en active Active
- 2007-08-07 PL PL07792065T patent/PL2050749T3/pl unknown
- 2007-08-07 ES ES07792065T patent/ES2657635T3/es active Active
- 2007-08-07 MY MYPI20090459A patent/MY145385A/en unknown
- 2007-08-07 AU AU2007282535A patent/AU2007282535B9/en active Active
- 2007-08-07 WO PCT/JP2007/065396 patent/WO2008018426A1/fr active Search and Examination
- 2007-08-07 JP JP2008528817A patent/JP4450857B2/ja active Active
- 2007-08-07 HU HUE07792065A patent/HUE035116T2/hu unknown
- 2007-08-07 CA CA2659604A patent/CA2659604C/fr active Active
- 2007-08-08 AR ARP070103510A patent/AR062292A1/es active IP Right Grant
- 2007-08-08 CL CL200702316A patent/CL2007002316A1/es unknown
- 2007-08-08 TW TW096129165A patent/TWI394758B/zh active
- 2007-08-08 PE PE2007001059A patent/PE20080527A1/es active IP Right Grant
-
2008
- 2008-10-28 NO NO20084533A patent/NO342978B1/no unknown
-
2009
- 2009-01-20 IL IL196601A patent/IL196601A/en active IP Right Grant
-
2017
- 2017-12-28 CY CY20171101353T patent/CY1119882T1/el unknown
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Legal Events
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FF | Patent granted | ||
KB | Patent renewed | ||
KB | Patent renewed | ||
KB | Patent renewed |